化合物 Resomelagon T60655

Product Introduction
Bioactivity


英文名: Resomelagon

描述: Resomelagon (AP1189) 是具有口服活性的有效黑素皮质素受体 (MR) 激动剂，可诱导Ca2+流动和 ERK1/2 磷酸化。Resomelagon 显示出抗炎活性， 可用于研究肥胖和慢性炎症。

体外活性: Resomelagon (AP1189) (0-1000 μM; 8 min; HEK293A cells) promotes melanocortin signal transduction through ERK1/2 phosphorylation and Ca 2+ mobilization [1]. Resomelagon (AP1189) (1 nM; 30 min; peritoneal macrophages) has anti-inflammatory activity and inhibits TNF-α release and efferocytosis [1]. Western Blot Analysis [1] Cell Line: HEK293A cells Concentration: 0-1000 μM Incubation Time: 8 minutes Result: Increased the expression of ERK1/2 phosphorylation in a dose-dependent manner.

体内活性: Resomelagon (AP1189) (0-10 mg/kg; i.p., i.v. and p.o.; for 24 h; male C57BL/6J wild-type (WT) and BALB/c mice) promotes resolution of acute inflammation in vivo [1]. Resomelagon (AP1189) (25-50 mg/kg; p.o.; daily, for 8 d; male C57BL/6J wild-type (WT) and BALB/c mice) reduces arthritis in mice [1]. Animal Model: Male C57BL/6J wild-type (WT) and BALB/c mice [1] Dosage: 0, 0.1, 1 and 10 mg/kg Administration: Oral administration, intraperitoneal injection and intravenous injection; for 24 hours Result: Inhibited neutrophil and monocyte infiltration in a dose-dependent manner. Animal Model: Male C57BL/6J wild-type (WT) and BALB/c mice [1] Dosage: 25 and 50 mg/kg Administration: Oral administration; daily; for 8 days Result: Reduced all signs of arthritis measured, including clinical score ( 42%), paw swelling ( 87%), proportion of animals with all four paws affected ( 50%), and the severity of the inflammation ( 70%).

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途